EP 0639573 A1 19950222 - Benzocondensed five membered heterocycles, process of their preparation, their use as drug, as diagnostic means and pharmaceuticals containing it.
Title (en)
Benzocondensed five membered heterocycles, process of their preparation, their use as drug, as diagnostic means and pharmaceuticals containing it.
Title (de)
Benzokondensierte 5-Ringheterocyclen, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament, ihre Verwendung als Diagnostikum, sowie sie enthaltendes Medikament.
Title (fr)
Hétérocycles à cinq chaînons benzocondensés, procédé pour leur préparation, leur utilisation comme médicament et comme diagnostique aussi bien que les produits pharmaceutiques le contenant.
Publication
Application
Priority
- DE 4326005 A 19930803
- DE 4414316 A 19940425
Abstract (en)
There are described benzo-fused 5-membered ring heterocycles of the formula I <IMAGE> where X is N or CR(6); Y is oxygen; A and B together are a bond or are both hydrogen if X is simultaneously CR(6) and Y is NR(7), one of these substituents R(1) to R(6) is a -CO-N = C(NH2)2 group; the other substituents R(1) to R(6) in each case are H, Hal, alkyl; up to two of the other substituents R(1) to R(6) are CN, NO2, N3, (C1-C4)-alkoxy, CF3; up to one of the other substituents is R(8)-CnH2n-Z-, phenyl; R(7) is H, alk(en)yl, R(8)-CnH2n-, and their pharmaceutically tolerable salts. There is further described a process for the preparation of the compounds I, which consists in reacting a compound of the formula II <IMAGE> wherein one of the substituents R(1)' to R(5)' is a -CO-L group and L is a leaving group which can be readily nucleophilically substituted, with guanidine, and in optionally converting the product to the pharmacologically tolerable salts.
Abstract (de)
Beschrieben werden benzokondensierte 5-Ringheterocyclen der Formel I <IMAGE> mit X gleich N oder CR(6); Y gleich Sauerstoff, S oder NR(7); A und B gemeinsam eine Bindung oder beide Wasserstoff, sofern gleichzeitig X gleich CR(6) und Y gleich NR(7) sind, einer der Substituenten R(1) bis R(6) eine -CO-N = C(NH2)2-Gruppe; die jeweils anderen Substituenten R(1) bis R(6) H, Hal, Alkyl; bis zu zwei der anderen Substituenten R(1) bis R(6) CN, NO2, N3, (C1-C4)-Alkyloxy, CF3; bis zu einem der anderen Substituenten R(8)-CnH2n-Z-, Phenyl; R(7) gleich H, Alk(en)yl, R(8)-CnH2n-, sowie deren pharmazeutisch verträgliche Salze. Beschrieben wird ferner ein Verfahren zur Herstellung der Verbindungen I, welches darin besteht, daß man eine Verbindung der Formel II <IMAGE> worin einer der Substituenten R(1)' bis R(5)' eine -CO-L -Gruppe bedeutet und L für eine leicht nucleophil substituierbare leaving group steht, mit Guanidin umsetzt, und daß man gegebenenfalls in das pharmakologisch verträgliche Salz überführt.
IPC 1-7
C07D 307/85; C07D 277/68; C07D 333/70; C07D 249/18; C07D 235/32; C07D 209/42; A61K 31/33
IPC 8 full level
A01N 1/02 (2006.01); A61K 31/34 (2006.01); A61K 31/343 (2006.01); A61K 31/38 (2006.01); A61K 31/381 (2006.01); A61K 31/40 (2006.01); A61K 31/403 (2006.01); A61K 31/404 (2006.01); A61K 31/41 (2006.01); A61K 31/415 (2006.01); A61K 31/4184 (2006.01); A61K 31/42 (2006.01); A61K 31/423 (2006.01); A61K 31/425 (2006.01); A61K 31/428 (2006.01); A61K 31/44 (2006.01); A61K 31/4427 (2006.01); A61K 31/4433 (2006.01); A61P 9/00 (2006.01); A61P 9/06 (2006.01); A61P 9/08 (2006.01); A61P 9/10 (2006.01); A61P 11/00 (2006.01); A61P 13/02 (2006.01); A61P 15/00 (2006.01); A61P 25/28 (2006.01); A61P 35/00 (2006.01); C07D 209/08 (2006.01); C07D 209/42 (2006.01); C07D 235/08 (2006.01); C07D 235/12 (2006.01); C07D 235/26 (2006.01); C07D 235/28 (2006.01); C07D 235/32 (2006.01); C07D 249/18 (2006.01); C07D 263/56 (2006.01); C07D 263/58 (2006.01); C07D 277/68 (2006.01); C07D 277/82 (2006.01); C07D 307/84 (2006.01); C07D 307/85 (2006.01); C07D 307/86 (2006.01); C07D 333/60 (2006.01); C07D 333/68 (2006.01); C07D 333/70 (2006.01); C07D 401/04 (2006.01); C07D 409/04 (2006.01)
CPC (source: EP KR)
A61P 9/00 (2017.12 - EP); A61P 9/06 (2017.12 - EP); A61P 9/08 (2017.12 - EP); A61P 9/10 (2017.12 - EP); A61P 11/00 (2017.12 - EP); A61P 13/02 (2017.12 - EP); A61P 15/00 (2017.12 - EP); A61P 25/28 (2017.12 - EP); A61P 35/00 (2017.12 - EP); C07D 209/42 (2013.01 - EP KR); C07D 235/32 (2013.01 - EP KR); C07D 249/18 (2013.01 - EP KR); C07D 277/68 (2013.01 - EP KR); C07D 307/85 (2013.01 - EP KR); C07D 307/86 (2013.01 - EP KR); C07D 333/70 (2013.01 - EP KR)
Citation (search report)
- [AD] EP 0416499 A2 19910313 - HOECHST AG [DE]
- [A] DE 4127026 A1 19930218 - BOEHRINGER INGELHEIM KG [DE]
- [A] WO 8400875 A1 19840315 - RORER INT OVERSEAS [US]
- [A] EP 0116360 A1 19840822 - KALI CHEMIE PHARMA GMBH [DE]
Designated contracting state (EPC)
AT BE CH DE DK ES FR GB GR IE IT LI LU NL PT SE
DOCDB simple family (publication)
EP 0639573 A1 19950222; AU 682371 B2 19971002; AU 6884494 A 19950216; CA 2129301 A1 19950204; CN 1118347 A 19960313; FI 943579 A0 19940801; FI 943579 A 19950204; HU 218790 B 20001228; HU 9402271 D0 19940928; HU T70547 A 19951030; IL 110503 A0 19941021; IL 110503 A 20000629; JP H07145149 A 19950606; KR 100343292 B1 20021226; KR 950005512 A 19950320; KR 950005817 A 19950320; NO 301584 B1 19971117; NO 942864 D0 19940802; NO 942864 L 19950206; NZ 264130 A 19951221
DOCDB simple family (application)
EP 94111765 A 19940728; AU 6884494 A 19940801; CA 2129301 A 19940802; CN 94109516 A 19940802; FI 943579 A 19940801; HU 9402271 A 19940803; IL 11050394 A 19940729; JP 19894094 A 19940802; KR 19940019071 A 19940802; KR 19940019259 A 19940802; NO 942864 A 19940802; NZ 26413094 A 19940729